High doses cause severe intoxication. Deterioration of the condition can be noticed by the appearance of symptoms of acute psychosis or severe depression of consciousness. Possible death due to respiratory paralysis, cardiac arrhythmias, convulsive syndrome.
All cases of overdose require immediate hospitalization in the intensive care unit or intensive care unit. The risk of side effects increases in people who are already taking sedatives or sleeping pills. Scopolamine also enhances the effect of painkillers, anticonvulsants and antihypertensive drugs, in theory - narcotic substances (more detailed studies are required).
Pharmacodynamics and pharmacokinetics
What is Scopolamine?
An organic nitrogen-containing compound found in datura, henbane, belladonna, and scopolia.
Pharmacodynamics
The M-anticholinergic effect manifests itself most clearly with hypertonicity of the parasympathetic nervous system or against the background of excitation of m-cholinergic receptors . In large doses, it can contribute to the development of tachycardia . Increases minute blood volume, improves conductivity and excitability of the myocardium. It has a ganglion-blocking and direct antispasmodic myotropic effect, dilates the peripheral blood vessels of the skin. In large doses, it suppresses the vasomotor center and inhibits the sympathetic ganglia, resulting in a decrease in pressure and dilation of blood vessels (when administered intravenously).
It reduces the secretion of secretions by the exocrine glands, causes a sharp decrease in the tone of smooth muscles, the frequency and amplitude of peristaltic movements of the stomach and intestines; with hyperkinesia , it weakens the tone of the walls of the gallbladder; with hypokinesia , it increases the tone of the gallbladder to a physiological level.
Relaxes the smooth muscles of the bladder, uterus and urinary tract, has an antispasmodic effect, and relieves pain . It also reduces the tone of the smooth muscles of the bronchial tree, increasing tidal volume, and suppresses the secretion of the bronchial glands.
When applied topically in the eye area and parenterally, it dilates the pupil and increases the pressure inside the eye. The effect on accommodation compared to atropine is less pronounced.
In large doses, Scopolamine can cause depression of the respiratory and vasomotor centers and convulsions.
Story
Scopolamine is one of the first alkaloids, isolated from plants in 1880 by the German scientist Albert Ladenburg. Scopolamine has been used in purified form (eg, various salts, including hydrochloride, hydrobromide, hydroiodide, and sulfate). The plant itself has been included in various medicinal preparations since ancient times. Following Ladenburg's description of the structure and activity of scopolamine, the search for synthetic analogues and methods for the total synthesis of scopolamine and/or atropine in the 1930s and 1940s led to the discovery of diphenhydramine, an early antihistamine and the prototype chemical subclass of these drugs, as well as pethidine, the first completely a synthetic opioid analgesic also known as Dolatin and Demerol. From 1900 until the 1960s, scopolamine was used in combination with morphine, oxycodone, or other opioids as an “anesthetic” for women in labor. The analgesia produced by scopolamine, when combined with a strong opioid, is powerful enough to allow higher doses of anesthesia to be used. Scopolamine, mixed with oxycodone (Eukodal) and ephedrine, was marketed as Merck's SEE (the name was derived from the German abbreviation of the main ingredients) and, beginning in 1928, as Scophedal. This mixture is sometimes mixed on site, most often in the areas of its wide historical use, namely Germany and Central Europe. Scopolamine was also one of the active ingredients in the drug Asthmador, sold over-the-counter in the 1950s and 60s as a drug to combat asthma and bronchitis when smoked. In November 1990, the US FDA initiated the withdrawal from the market of over-the-counter drugs containing scopolamine and several hundred other ingredients that were allegedly not proven to be effective. Scopolamine shared a small segment of the over-the-counter sedative market with Diphenhydramine, Phenyltoloxamine, Pyrilamine, Doxylamine and other first-generation antihistamines, many of which are still used for this purpose today in drugs such as Sominex, Tylenol PM, NyQuil and etc.
Indications for use
- Vegetovascular dystonia;
- Parkinson's;
- Meniere's disease;
- as a premedication;
- psychomotor agitation;
- vomit;
- hypersalivation;
- to dilate the pupil when examining the fundus of the eye and determining ocular refraction;
- eye injuries;
- iritis, keratitis, iridocyclitis;
- prevention of sea and air sickness.
This is dope?
Scopolamine - what is it: a medicine or a drug? It depends on the purpose of use and dosage. In small doses, the drug really helps doctors fight certain ailments of patients. However, if taken uncontrolled, the drug becomes addictive. Moreover, it is considered one of the most dangerous drugs in the world, as it deprives a person of willpower and memory.
In the world of drug addicts it is also called “devil’s breath.” The drug turns a person into a zombie. Consciousness is temporarily switched off, the victim does not perceive reality, and does what he is told. After the drug wears off, people do not remember what happened to them during this period, since it blocks the flow of information into short-term memory.
In the early twentieth century, the alkaloid was used by intelligence agencies as a "truth serum." For criminal purposes it is used for sexual violence, robbery, kidnapping. The substance is colorless, odorless and tasteless, so it is very easy to sneak it into the victim. Victims often do not remember what happened to them while the drug was in effect, so they are embarrassed to contact the police.
The stages of exposure to excessive doses of the drug in clinical studies are described as follows:
- dilated pupils, redness of the skin on the arms and legs, slurred speech;
- loss of strength, impaired movement, increased heart rate, delirium;
- complete loss of strength, inability to get up, hearing impairment, pupils dilate greatly, spatial orientation disturbance;
- hallucinations, reality is completely distorted;
- sensations as if the person is paralyzed, he does not understand where he is and what is happening to him;
- after the end of the effect of the substance, consciousness gradually returns to normal, motor and auditory activity is restored.
The period of disorientation and unconsciousness, as well as the severity of symptoms, depend on the dosage taken.
Contraindications
Sensitization to the drug Scopolamine.
Caution should be prescribed for diseases of the circulatory system accompanied by tachycardia ; thyrotoxicosis ; reflux esophagitis; hyperthermia; hernia due to reflux esophagitis ; diseases of the digestive system, accompanied by obstruction; diseases with increased intraocular pressure; nonspecific ulcerative colitis ; dry mouth; renal failure ; chronic lung diseases; myasthenia gravis ; prostate hypertrophy without obstructive phenomena; autonomic neuropathy ; urinary retention and obstructive urinary tract diseases; gestosis ; brain damage in children, Down's disease and central palsy in children.
How to get rid of addiction?
Dependence is caused by the sedative and hallucinogenic properties of the drug. It should be noted that reactions to it may vary from person to person. Some people have terrible nightmares, while others have vivid pictures accompanied by a feeling of euphoria. A person can also become a victim of criminals who add powder to carry out their criminal plans. In all these cases, the victim needs medical and psychological help.
The alkaloid is very toxic and has a destructive effect on brain cells. Long-term use leads to acute mental disorders, including complete personality degradation. Hot temper and aggression worsen, and over time, unreasonable anxiety and paranoia develop. Suicide attempts are possible. The heart, digestive system, kidneys, liver, and brain are most affected.
Treatment must be comprehensive. To return to a full life, a course is required that includes detoxification, psychotherapy, biomolecular restoration, and kinesiogenic practices. You can get all this at the IMC Addiction By Yuzapolsky clinic. A team of specialists with many years of experience will help you forget about the horrors of addiction forever and return to a happy, sober life.
Side effects
- Thirst and dry mouth;
- decrease in pressure;
- paralysis of accommodation;
- mydriasis;
- atony ;
- tachycardia;
- drowsiness and dizziness ;
- impaired concentration and slowing of psychomotor reactions, acute psychosis;
- headache;
- convulsions;
- photophobia;
- urinary retention.
Text
USSR M 60093 Class 12 r, 13 IYA DESCRIPTION OF BR TO AUTHOR'S CERTIFICATE Registered in the Department of Ieobregpeniya Gosplan under the State Tax Committee GS ng, ",.- ,.-,.,"4 f 1,1, ; 1,1,.;.;."-.s:;: Shchukina, S.S. Okun and D. Nob received January 1-20, 1940, published May 31, 1941. rygin. scopolamine, NKZdrav aa3196. Declarate and isolate a new portion of the 1-isomer using the method described above. For example, 100 g of racemic scopolavine (base) is mixed with 60 g of camphoric acid and dissolved in 100 ml of boiling water. With rapid cooling and constant stirring, a white crystalline precipitate of 1-scopolamine o-bicampharate, composition C, H. O, X 2 (CHO,) gradually precipitates from the solution. , ,After standing in the cold for 24 hours, the sediment is sucked off and washed thoroughly. Yield of dry salt 64 g, melting temperature 151. By means of repeated recrystallization of scopolamine salt and a - bromo-p-sulfonic acid, isolate a small amount of d-scopolamine salt with this acid, and from it with 1-scopolamine. Authors of the present invention propose to obtain 1-scopolamine from the racemate, taking advantage of the poor solubility of the salt from 1-scopolamine c a-camphoric acid. After the reaction, the salt containing the 1-isomer is filtered off, and the 4-isomer remaining in the filtrate can easily be re-raced. In some productions it is scopolia root. This root, along with hyoscyamine, also contains scopolamine in the form of the levorotatory isomer. During the production process, scopolamine accumulates in the mother liquors and upon further purification is largely racemized
In view of the fact that 1-scopolamine is the most valuable in the pharmacopoeia, it is very important to separate the racemate into isomers. Attempts to separate racemic scopolamine have been made repeatedly. Thus, King succeeded in recrystallization from 140 ml of boiling water to obtain 48 g of pure 1-scopolamine bicampharate with a melting point of 155 in 1. The combined mother liquors are treated again with 60 g of a-camphoric acid, which gives another 40 g of recrystallized bicampharate. Upon receipt of this salt in a more concentrated solution, the yield is much greater, but the quality of the product is lower and three to fourfold crystallization is required for purification. Bicampharate is transferred in the osiobath of 1-scopolamine by adding sodium bicarbonate and extragyrone: adding chloroform
The resulting base of 1-scopolamine after distilling off chloroform is converted in a known manner to 1-scopolamine bromine hydrate. It has a melting point of 192 in 1 and shows a specific rotation corresponding to the pure preparation scolopaminac n = - 25.82. And the solution solutions from the isolation of = - camphorate 1- Scopolamine is used to release additional amounts as follows. the solutions are acidified with hydrochloric acid to release camphoric acid. Then, after sucking off the latter, the filtrate is treated with bicarbonate and a mixture of racemic and right scopolamine is extracted from it with chloroform. This base is dissolved in four times the amount of methyl alcohol and 106 norms are added to the solution. a small alcohol solution of sodium methoxide. At O - 5, complete racemization is achieved within 3 hours. The progress of racemization is monitored by determining the rotation in a nolarimeter. From the solution of racemic scopolamine obtained in this way, 1-scopolamine is isolated by adding an equal amount of camphoric acid. Subject of the invention: A method for obtaining 1-scopolamine from racemic by crystallization in an aqueous solution of its salts with camphor derivatives obtained in the usual way, from t and the reason is that the salts of scopolamine with k-camphoric acid are subjected to crystallization and the poorly soluble salt of 1-scopolamine with camphoric acid is separated from the solution of the salt of the other antipode using known methods,
Look
Overdose
Symptoms: acute urinary retention , intestinal obstruction caused by paralysis of smooth muscles, paralysis of accommodation and severe mydriasis , increased pressure inside the eye, dry mucous membranes of the oropharynx, impaired swallowing and speech, convulsions, tremor, hyperthermia, depression or excitation of the nervous system, depression of the vasomotor and respiratory centers .
Therapy: gastric lavage, parenteral administration of anticholinesterase drugs and anticholinergic stimulants, symptomatic treatment.
Biosynthesis in plants
Scopolamine biosynthesis begins with the decarboxylation of L-ornithine to putrescine via ornithine decarboxylase (EC 4.1.1.17). Putrescine is methylated to N-methylputrescine via putrescine N-methyltransferase (EC 2.1.1.53). Putrescine oxidase (EC 1.4.3.10) specifically targets methylated putrescine and catalyzes the deamination of this compound to 4-methylaminobutanal, which then spontaneously forms a ring with the N-methyl-pyrrole cation. In the next step, the pyrrole cation condenses with acetoacetic acid, resulting in the formation of hygrine. This reaction is not catalyzed by any enzymatic activity. Hygrin is subsequently rearranged into tropinone. Tropinone is subsequently converted by tropinone reductase I (EC 1.1.1.206) to tropine, which condenses with phenylalanine-derived phenyllactate to form littorine. Cytochrome P450, classified as Cyp80F1, is oxidized and converts littorine to hyoscyamine aldehyde. In the final step, hyoscyamine undergoes epoxidation, catalyzed by 6 beta-hydroxyhyoscyamine epoxidase (EC 1.14.11.14), resulting in the formation of scopolamine.
Interaction
The drug may provoke an increase in the sedative and hypnotic effects of magnesium sulfate, phenobarbital, sodium etaminal and increase the possibility of developing undesirable manifestations when taken together with MAO inhibitors , Amantadine , Phenothiazine , Haloperidol, tricyclic antidepressants.
Scopolamine enhances the effect of anxiolytic drugs, sedatives, analgesics, tranquilizers in the treatment of pain caused by spasms .
It should not be used for the treatment and prevention of kinetosis in combination with other drugs.
Interesting Facts
Thanks to its wide history, many interesting facts have accumulated around scopolamine:
- the appearance of hallucinations was often perceived as magic. Because of this, the plant began to be actively used to perform magical rituals, witches’ Sabbaths and similar events;
- it was used as a means to obtain secret information. Without unnecessary torture, the victim could tell all the secrets;
- the drug was used by the CIA;
- Due to its anti-nausea effect, it is prescribed to astronauts in combination with other medications.
Thus, it is difficult to draw clear conclusions. There are many conflicting opinions around the plant. For some it is a benefit, but for others it can cause many serious problems.
https://youtube.com/watch?v=Y5TfF9VYbzY
Scopolamine
(Scopolaminum). An alkaloid found together with atropine in belladonna, henbane, datura, and scopolia. It is used in the form of scopolamine hydrobromide (socopolamine hydrobromidum). Synonyms: Scopolaminum hydrobromicum, Hyoscini hydrobromidum. Colorless transparent crystals or white crystalline powder. Easily soluble in water (1:3), soluble in alcohol (1:17). In order to stabilize injection solutions, add a solution of hydrochloric acid to pH 2.8-3.0. Sterilize at + 100 C for 30 minutes. Chemically, scopolamine is close to atropine: it is an ester of scopine and tropic acid. Close to atropine in its effect on peripheral cholinoreactive systems. Like atropine, it causes dilation of the pupils, paralysis of accommodation, increased heart rate, relaxation of smooth muscles, and a decrease in the secretion of the digestive and sweat glands.
It also has a central anticholinergic effect. Usually causes a sedative effect: reduces motor activity, may have a hypnotic effect. A characteristic property of scopolamine is the amnesia it causes. Scopolamine is sometimes used in psychiatric practice as a sedative, in neurological practice for the treatment of parkinsonism, in surgical practice along with analgesics (morphine, promedol) - to prepare for anesthesia, sometimes as an antiemetic and sedative for sea and air sickness (more often for this Aeron tablets are prescribed for this purpose), as well as for iritis, iridocyclitis and for diagnostic purposes to dilate the pupil instead of atropine. Contraindications are the same as when prescribing atropine. It is necessary to take into account the very wide variation in individual sensitivity to scopolamine: relatively often, usual doses do not cause sedation, but agitation, hallucinations and other side effects. Scopolamine is prescribed orally (usually in solutions and under the skin in single doses of 0.00025-0.0005 g (0.25 - 0.5 mg) or 0.5-1 ml of 0.05% solution. In ophthalmic practice (for dilation pupil and paralysis of accommodation) use a 25% aqueous solution (1 - 2 drops in the eyes 2 times a day) or 0.25% ointment Higher doses for adults orally and subcutaneously: single dose 0.0005g , daily 0.0015 g. Forms of release: powder; 0.05% solution in ampoules of 1 ml. In ophthalmic practice, along with a 0.25% aqueous solution, a prolonged preparation is used - a solution of scopolamine hydrobromide 0.25% with methylcellulose (Solutio Scorolamini hidrobromidi 0.25% cum Methylcelluloso).Colorless transparent or slightly opalescent liquid (pH 4.5 - 6.5) in bottles of 5 and 10 ml. Storage: list A. In a well-closed container, protected from light. Rр. : Sol. Scopolamini hydrobromidi 0.05% 1 ml DtdN 6 in ampull. DS Po O.5 - 1 ml under the skin Rp.: Scopolamini hydrocarbomidi 0.0025 Promedoli O.1 Ephedrini hydrochloridi 0.125 ml Aq. rgo inject. 5 ml M. Steril.! DS 1 ml subcutaneously or intramuscularly as an anesthetic for injuries; for induction anesthesia Rp.: Sol. Scopolamini hydrobromidi 0.25% 10 ml DS Eye drops. 1 - 2 drops 3-4 times a day (for iridocyclitis)
Note: It is not allowed to take a solution of this concentration orally or inject it under the skin. Tablets "Aeron" (Tabulettae "Aeronum"). Composition: scopolamine camphorate 0.0001 g and hyoscyamine camphorate 0.0004 g. The action of the tablets is associated with the pharmacodynamics of scopolamine and hyoscyamine. Aeron tablets are used for the prevention and treatment of sea and air sickness, as well as for the prevention and relief of attacks of Meniere's disease [see. also Dimenhydrate (Dedalon)]. Sometimes they are used to reduce mucus and salivation during plastic surgery on the face and during operations on the upper respiratory tract. For air and sea sickness, tablets are prescribed orally: prophylactically, 30-60 minutes before departure, take 1-2 tablets, and then, if necessary, after 6 hours, take another tablet. If aeron was not used prophylactically, then at the first signs of illness (nausea, dizziness, headache) take 1-2 tablets, then give one tablet 2 times a day. Higher doses for adults: single dose 2 tablets, daily dose 4 tablets. In rare cases, with persistent vomiting, suppositories containing as much scopolamine camphorate and hyoscyamine as are contained in one Aeron tablet may be prescribed instead of Aeron. For Meniere's disease, 1 tablet is prescribed 2-3 times a day. For surgical interventions on the face, 2 tablets are prescribed immediately 20-30 minutes before surgery and after surgery, 1 tablet 2 times a day for the first 2 days. When using Aeron, thirst, dry mouth and throat are possible. To alleviate this condition, drinks and caffeine are prescribed. The tablets should not be prescribed to patients with glaucoma. Release form: tablets of 0.0005 g in a package of 10 pieces. Storage: list B.
Scopolamine Great Medical Encyclopedia Vol. 1 volume 30
Scopolamine, Scopolaminum, FUP, an alkaloid similar in chemical properties. composition and structure to atropine and in small quantities found along with it in various plants of the family. nightshades (datura, henbane, belladonna, etc.). Having been primarily discovered (in an impure form) in henbane and taken as an isomer of hyoscyamine, S. received the name hyoscine (Hyo-scinum), which is still occasionally used. S., having the composition C17H21NO4, is an ester of scopolin and tropic acid. Crystalline S. contains one particle of water, amorphous does not contain water, melts at 59°. S. is difficult to dissolve in water and easily in alcohol, ether, and chloroform. When boiled, S. decomposes into scopoline and tropic acid. Possessing significant optical activity (rotates to the left), it is inactivated by caustic alkalis, turning into the racemic form (Atroscin), which is 2-4 times less toxic than levorotatory. Easily forms crystalline salts with compounds (of which bromide is the official one), which are readily soluble in acidic water. Absorption, excretion and destruction of S. occur much faster than atropine, which is why the pharmacological effect, while occurring faster, also passes faster. The peripheral effect of S. is characterized by paralysis of the endings of the parasympathetic nervous system, similar to atropine. It is used therapeutically. arr. in order to dilate the pupil. Resorptive effect on the endings of the parasympathetic nervous system during therapy. doses of S. are insignificant.
The main difference between S. and atropine is its effect on the central nervous system. Doses of 0.3-0.5 mg cause a person to feel tired, unwilling to move, difficulty speaking and unsteady gait, sometimes dizziness and headaches; then drowsiness develops and after about 1 hour sleep lasts 5-8 hours. Scopolamine sleep is more sensitive than chloral sleep, and upon awakening consciousness is clearer; upon awakening, the depressive effect of S. on the motor sphere still lasts for several hours, and dry throat and thirst are often felt. Doses of 1-2 mg lead to mental and motor agitation. With large doses, convulsions occur, the pupils dilate, and the skin becomes dry and red. Unlike atropine, scopolamine not only does not excite, but in large doses even depresses breathing. The most characteristic effect of scopolamine is sedation of the central nervous system, which is mainly used in therapy.
Main indications: 1. State of motor excitation in mental patients. S.'s dosage in the latter is usually higher than in mentally healthy people. With repeated use, you have to increase the dose (twice after two weeks). S. does not cause addiction in the sense of drug addiction. When prescribed during the day, S. may not reduce, but even increase agitation. 2. Hyperkinesis with shaking paralysis and postencephalic parkinsonism (also chorea, senile tremors, etc.). In addition to the suppression of convulsive movements and contractures, after S. there is an improvement in speech, a weakening of salivation and lacrimation. S.'s dosage in these cases is 0.4 mg subcutaneously and up to 1-2 mg per day. S. gives the best effect here
better than atropine, which is often used for the same indications. 3. Marine b-n. In therapy, S.'s synergism with other pharmacological agents acting on the central nervous system is sometimes used, for example: a) with ether (ether-scopolamine anesthesia); b) with opiates [morphine (0.01), pantopon (0.02)], in order to enhance the sedative effect or obtain anesthesia (morphine-scopolamine anesthesia); c) with sleeping pills. An enhanced effect is obtained when combined with substances that primarily inhibit subcortical functions (luminal, pernoctone), which, along with other data, confirms the opinion about the subcortical localization of the action of Solanaceae alkaloids. When S. is combined with hypnotics that act primarily on the cortex, the effect is slightly enhanced (chloral hydrate) or absent (paraldehyde). 4. Like mydriaticum, e.g. for iritis, in doses five times less than atropine: one drop of solution 1-2: 1,000.— Preparations: 1) Scopolaminum
hydrobromicum. The highest single dose is 0.0005, the highest daily dose is 0.0015 (F VII);
- 2) A t r o s cinum hydrobromicum;
- 3) Duboisinu m—a mixture of S. and hyoscyamine. Treatment of S. poisoning, according to the literature, does not differ from the treatment of atropine poisoning.
Lit.: Lobasov, On the issue of the influence of Scopolamini hydrobromici on the eye, diss., St. Petersburg, 1893; Pavlov K., Materials for the pharmacology of hyoscine hydrochloride, diss., St. Petersburg, 1889; Spirin I., On the effect of atroscine on the eye, dissertation, St. Petersburg, 1907; Friedberg Ch., Uber die verstarkende Wirkung des Atropins, Scopolamine und Hyosciamins auf verschiedene Schlafmittel, Arch. f. exp. Pathol, u. Pharmakoi., B. CLX, 1931; Mehes J., Stu-dien fiber den Scopolaminschlaf und seine Verstarkung durch Morphium, ibid., B. CXLII, 1929. V. Karasik.
Scopolamine hydrobromide:
Scopolamine hydrobromide (Scopolamini hydrobromidum) is a crystalline white powder, easily soluble in water. The drug is prescribed orally and under the skin. In ophthalmic practice, a 0.25% aqueous solution of scopolamine hydrobromide is used.
Single doses of the drug: 0.00025–0.0005 g (0.25–0.5 mg) or 0.5–1 ml of 0.05% solution. Higher doses of scopolamine for adults orally and subcutaneously: single 0.0005 g, daily 0.0015 g.
The drug scopolamine hydrobromide is available in powder form and in ampoules of 1 ml of 0.05% solution.
Store scopolamine in well-sealed orange glass jars in a dry place, protected from light.
